For research use only. Not for therapeutic Use.
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment[1][2].
LS-102 inhibits proliferation of RSCs with an IC50 of 5.4 μM[1].
LS-102 suppresses proliferation of rheumatoid synovial cells (RSCs) in a Syvn1-dependent manner. LS-102 suppresses polyubiquitination of target proteins of Syvn1, including nuclear factor erythroid 2-related factor 2 (NRF2), V247M α-sarcoglycan mutant, and PGC-1β. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1)[2].
LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model[1].
| Catalog Number | I016817 |
| CAS Number | 1456891-34-1 |
| Synonyms | 6-N-(1,3-benzoxazol-6-yl)-4-N-[(1S)-1-cyclohexylethyl]-2-N-ethyl-2-N-[2-(ethylamino)ethyl]-1,3,5-triazine-2,4,6-triamine |
| Molecular Formula | C24H36N8O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H36N8O/c1-4-25-13-14-32(5-2)24-30-22(27-17(3)18-9-7-6-8-10-18)29-23(31-24)28-19-11-12-20-21(15-19)33-16-26-20/h11-12,15-18,25H,4-10,13-14H2,1-3H3,(H2,27,28,29,30,31)/t17-/m0/s1 |
| InChIKey | DEDHMXBDEJSZFE-KRWDZBQOSA-N |
| SMILES | CCNCCN(CC)C1=NC(=NC(=N1)NC(C)C2CCCCC2)NC3=CC4=C(C=C3)N=CO4 |
| Reference | [1]. Yagishita N, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoidarthritis. Int J Mol Med. 2012 Dec;30(6):1281-6. [2]. Fujita H, et al. Identification of the inhibitory activity of walnut extract on the E3 ligase Syvn1. Mol Med Rep. 2018 Dec;18(6):5701-5708. |
